降胆固醇药物新靶标前蛋白转化酶枯草溶菌素9的研究进展

发布时间：2018-05-07 07:42

本文选题：胆固醇代谢 + 低密度脂蛋白胆固醇　；参考：《第二军医大学学报》2017年11期

【摘要】：他汀类药物主要用于降低血低密度脂蛋白胆固醇(LDL-C)以及预防心血管疾病,但其临床疗效和机体的耐受性尚存在不稳定性。人类前蛋白转化酶枯草溶菌素9(PCSK9)属于前蛋白转化酶家族,主要由肝脏产生并分泌入血,可促进肝脏中低密度脂蛋白受体(LDLR)的降解,从而参与调控血LDL-C水平。人群中PCSK9的功能获得型或缺失型基因突变与血LDL-C含量、心血管疾病患病率密切相关。可通过负反馈机制上调PCSK9,促进LDLR的降解,从而降低他汀类药物的疗效。因此,抑制PCSK9活性可望成为治疗高胆固醇血症的一种新的有效方法。本文主要综述PCSK9调节胆固醇代谢及其临床应用的研究进展。
[Abstract]:Statins are mainly used to reduce LDL-C and prevent cardiovascular disease, but the clinical efficacy and tolerance are still unstable. Human proprotein converting enzyme lysogenin 9 (PCSK9) belongs to the proprotein converting enzyme family, which is mainly produced and secreted into blood by the liver, which can promote the degradation of low density lipoprotein receptor (LDLR) in the liver and thus participate in the regulation of blood LDL-C level. The mutation of PCSK9 functional acquisition type or deletion type gene is closely related to the blood LDL-C content and the prevalence of cardiovascular disease. PCSK9 can be upregulated by negative feedback mechanism to promote the degradation of LDLR and reduce the efficacy of statins. Therefore, inhibition of PCSK9 activity is expected to be a new and effective method for the treatment of hypercholesterolemia. This article reviews the progress in the regulation of cholesterol metabolism by PCSK9 and its clinical application.
【作者单位】：第二军医大学基础医学部病理生理学教研室;
【基金】：国家重点基础研究发展计划(“973计划”,2013CB530603) 国家自然科学基金(31730042)~~
【分类号】：R96

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